REBOPAG 25

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. Definition & Pharmacological Class

  • Generic Name: Eltrombopag olamine

  • Therapeutic Category: Thrombopoietin receptor agonist (TPO-RA)

  • Mechanism of Action:

    • Binds to transmembrane domain of TPO receptor

    • Stimulates JAK2/STAT5 pathway → megakaryocyte proliferation

    • Increases platelet production in bone marrow

2. Approved Indications

✅ FDA/EMA Approved Uses:

  1. Chronic Immune Thrombocytopenia (ITP)

    • Adults and children ≥1 year

    • Second-line after corticosteroids/IVIG failure

  2. Severe Aplastic Anemia (SAA)

    • In combination with immunosuppressants

  3. Hepatitis C-Associated Thrombocytopenia

    • Enables interferon-based antiviral therapy

🚫 Important Limitations:

  • Not for first-line ITP treatment

  • Contraindicated in myelodysplastic syndromes

  • Not approved for chemotherapy-induced thrombocytopenia

3. Pharmacokinetics

Parameter Value Clinical Significance
Bioavailability 52% Reduced with food
Tmax 2-6 hours Take on empty stomach
Half-life 26-35 hours Once daily dosing
Protein binding >99% Caution in hepatic impairment
Metabolism Hepatic (CYP1A2/CYP2C8) Drug interaction potential
Excretion Fecal (59%), renal (31%) Dose adjustment not needed for renal impairment

4. Dosage & Administration

Standard Dosing Guidelines:

Indication Starting Dose Titration Maximum Dose
Adult ITP 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (6-17 yrs) 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (1-5 yrs) 12.5 mg once daily ↑ by 12.5 mg every 2 weeks 75 mg/day
SAA 50 mg once daily* Adjust based on response 150 mg/day
HCV Thrombocytopenia 25 mg once daily ↑ weekly as needed 100 mg/day

Administration Instructions:

  • Take 1 hour before or 2 hours after meals

  • Avoid concomitant:

    • Dairy products (separate by ≥4 hours)

    • Polyvalent cation-containing medications (antacids, iron supplements)

  • Swallow tablet whole with water

5. Special Populations

Hepatic Impairment:

  • Mild (Child-Pugh A): Reduce starting dose by 50%

  • Moderate (Child-Pugh B): Reduce starting dose by 75%

  • Severe (Child-Pugh C): Contraindicated

Ethnic Considerations:

  • East Asian patients: Start at 50% reduced dose

  • Consider genetic testing for UGT1A1 polymorphisms

Pediatric Use:

  • Safety established down to 1 year old

  • Use oral suspension for children <25 kg

6. Adverse Effects

Common (≥10%):

  • Headache (22%)

  • Nausea (13%)

  • Fatigue (12%)

  • Upper respiratory infection (11%)

  • ALT elevation (10%)

Serious (Require Monitoring):

  • Hepatotoxicity (2.5%)

  • Thromboembolism (3%)

  • Bone marrow fibrosis (long-term use)

  • Cataract formation

7. Drug Interactions

Interacting Drug Effect Management
Polyvalent cations (Ca, Mg, Al, Fe) ↓ Absorption Separate by 4+ hours
CYP1A2 inhibitors (fluvoxamine) ↑ Eltrombopag levels Monitor for toxicity
CYP2C8 inducers (rifampin) ↓ Efficacy Consider dose increase
Statins ↑ Myopathy risk Monitor CK levels

8. Monitoring Requirements

Baseline:

  • CBC with platelet count

  • Liver function tests

  • Renal function

  • Ophthalmologic exam

  • Bone marrow biopsy (if long-term use anticipated)

Ongoing:

  • Weekly platelet counts until stable

  • LFTs every 2 weeks ×2 months, then monthly

  • Regular blood pressure monitoring

  • Annual:

    • Eye exams

    • Bone marrow evaluation (if chronic use)

9. Storage & Handling

  • Store at 20-25°C (68-77°F)

  • Keep in original packaging (moisture sensitive)

  • Protect from light

  • Shelf life: 24 months unopened

10. Cost & Availability

  • Brand Name Cost: ~$4,500/month

  • Generic Availability: Limited (check local formularies)

  • Patient Assistance Programs: Available through manufacturer

11. Clinical Pearls

  1. Dose Adjustment Triggers:

    • Platelets >150,000/μL: Reduce dose

    • Platelets >400,000/μL: Hold dose

    • No response after 4 weeks: Discontinue

  2. Transitioning Between Formulations:

    • 25 mg tablet ≈ 24 mg oral suspension

    • Monitor platelets closely when switching

  3. Overdose Management:

    • Symptomatic treatment

    • Monitor for thrombocytosis

    • Consider plateletpheresis if platelets >1,000,000/μL

  4. Discontinuation Protocol:

    • Taper gradually to avoid thrombocytopenia rebound

    • Monitor platelets for ≥4 weeks post-discontinuation

. Definition & Pharmacological Class

  • Generic Name: Eltrombopag olamine

  • Therapeutic Category: Thrombopoietin receptor agonist (TPO-RA)

  • Mechanism of Action:

    • Binds to transmembrane domain of TPO receptor

    • Stimulates JAK2/STAT5 pathway → megakaryocyte proliferation

    • Increases platelet production in bone marrow

2. Approved Indications

✅ FDA/EMA Approved Uses:

  1. Chronic Immune Thrombocytopenia (ITP)

    • Adults and children ≥1 year

    • Second-line after corticosteroids/IVIG failure

  2. Severe Aplastic Anemia (SAA)

    • In combination with immunosuppressants

  3. Hepatitis C-Associated Thrombocytopenia

    • Enables interferon-based antiviral therapy

🚫 Important Limitations:

  • Not for first-line ITP treatment

  • Contraindicated in myelodysplastic syndromes

  • Not approved for chemotherapy-induced thrombocytopenia

3. Pharmacokinetics

Parameter Value Clinical Significance
Bioavailability 52% Reduced with food
Tmax 2-6 hours Take on empty stomach
Half-life 26-35 hours Once daily dosing
Protein binding >99% Caution in hepatic impairment
Metabolism Hepatic (CYP1A2/CYP2C8) Drug interaction potential
Excretion Fecal (59%), renal (31%) Dose adjustment not needed for renal impairment

4. Dosage & Administration

Standard Dosing Guidelines:

Indication Starting Dose Titration Maximum Dose
Adult ITP 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (6-17 yrs) 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (1-5 yrs) 12.5 mg once daily ↑ by 12.5 mg every 2 weeks 75 mg/day
SAA 50 mg once daily* Adjust based on response 150 mg/day
HCV Thrombocytopenia 25 mg once daily ↑ weekly as needed 100 mg/day

Administration Instructions:

  • Take 1 hour before or 2 hours after meals

  • Avoid concomitant:

    • Dairy products (separate by ≥4 hours)

    • Polyvalent cation-containing medications (antacids, iron supplements)

  • Swallow tablet whole with water

5. Special Populations

Hepatic Impairment:

  • Mild (Child-Pugh A): Reduce starting dose by 50%

  • Moderate (Child-Pugh B): Reduce starting dose by 75%

  • Severe (Child-Pugh C): Contraindicated

Ethnic Considerations:

  • East Asian patients: Start at 50% reduced dose

  • Consider genetic testing for UGT1A1 polymorphisms

Pediatric Use:

  • Safety established down to 1 year old

  • Use oral suspension for children <25 kg

6. Adverse Effects

Common (≥10%):

  • Headache (22%)

  • Nausea (13%)

  • Fatigue (12%)

  • Upper respiratory infection (11%)

  • ALT elevation (10%)

Serious (Require Monitoring):

  • Hepatotoxicity (2.5%)

  • Thromboembolism (3%)

  • Bone marrow fibrosis (long-term use)

  • Cataract formation

7. Drug Interactions

Interacting Drug Effect Management
Polyvalent cations (Ca, Mg, Al, Fe) ↓ Absorption Separate by 4+ hours
CYP1A2 inhibitors (fluvoxamine) ↑ Eltrombopag levels Monitor for toxicity
CYP2C8 inducers (rifampin) ↓ Efficacy Consider dose increase
Statins ↑ Myopathy risk Monitor CK levels

8. Monitoring Requirements

Baseline:

  • CBC with platelet count

  • Liver function tests

  • Renal function

  • Ophthalmologic exam

  • Bone marrow biopsy (if long-term use anticipated)

Ongoing:

  • Weekly platelet counts until stable

  • LFTs every 2 weeks ×2 months, then monthly

  • Regular blood pressure monitoring

  • Annual:

    • Eye exams

    • Bone marrow evaluation (if chronic use)

9. Storage & Handling

  • Store at 20-25°C (68-77°F)

  • Keep in original packaging (moisture sensitive)

  • Protect from light

  • Shelf life: 24 months unopened

10. Cost & Availability

  • Brand Name Cost: ~$4,500/month

  • Generic Availability: Limited (check local formularies)

  • Patient Assistance Programs: Available through manufacturer

11. Clinical Pearls

  1. Dose Adjustment Triggers:

    • Platelets >150,000/μL: Reduce dose

    • Platelets >400,000/μL: Hold dose

    • No response after 4 weeks: Discontinue

  2. Transitioning Between Formulations:

    • 25 mg tablet ≈ 24 mg oral suspension

    • Monitor platelets closely when switching

  3. Overdose Management:

    • Symptomatic treatment

    • Monitor for thrombocytosis

    • Consider plateletpheresis if platelets >1,000,000/μL

  4. Discontinuation Protocol:

    • Taper gradually to avoid thrombocytopenia rebound

    • Monitor platelets for ≥4 weeks post-discontinuation

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Bulk Orders: You are responsible for any local import duties and taxes in your country.

For Patients: When ordering prescription medicines for personal use, or for a friend or relative, a valid medical practitioner’s script or prescription is required.

Return and Refund Policy: Due to the nature of our products, we cannot accept returns or exchanges once a purchase is made. However, in the event of non-delivery, you are eligible for either a 100% refund or a reshipment of your order.

. Definition & Pharmacological Class

  • Generic Name: Eltrombopag olamine

  • Therapeutic Category: Thrombopoietin receptor agonist (TPO-RA)

  • Mechanism of Action:

    • Binds to transmembrane domain of TPO receptor

    • Stimulates JAK2/STAT5 pathway → megakaryocyte proliferation

    • Increases platelet production in bone marrow

2. Approved Indications

✅ FDA/EMA Approved Uses:

  1. Chronic Immune Thrombocytopenia (ITP)

    • Adults and children ≥1 year

    • Second-line after corticosteroids/IVIG failure

  2. Severe Aplastic Anemia (SAA)

    • In combination with immunosuppressants

  3. Hepatitis C-Associated Thrombocytopenia

    • Enables interferon-based antiviral therapy

🚫 Important Limitations:

  • Not for first-line ITP treatment

  • Contraindicated in myelodysplastic syndromes

  • Not approved for chemotherapy-induced thrombocytopenia

3. Pharmacokinetics

Parameter Value Clinical Significance
Bioavailability 52% Reduced with food
Tmax 2-6 hours Take on empty stomach
Half-life 26-35 hours Once daily dosing
Protein binding >99% Caution in hepatic impairment
Metabolism Hepatic (CYP1A2/CYP2C8) Drug interaction potential
Excretion Fecal (59%), renal (31%) Dose adjustment not needed for renal impairment

4. Dosage & Administration

Standard Dosing Guidelines:

Indication Starting Dose Titration Maximum Dose
Adult ITP 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (6-17 yrs) 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (1-5 yrs) 12.5 mg once daily ↑ by 12.5 mg every 2 weeks 75 mg/day
SAA 50 mg once daily* Adjust based on response 150 mg/day
HCV Thrombocytopenia 25 mg once daily ↑ weekly as needed 100 mg/day

Administration Instructions:

  • Take 1 hour before or 2 hours after meals

  • Avoid concomitant:

    • Dairy products (separate by ≥4 hours)

    • Polyvalent cation-containing medications (antacids, iron supplements)

  • Swallow tablet whole with water

5. Special Populations

Hepatic Impairment:

  • Mild (Child-Pugh A): Reduce starting dose by 50%

  • Moderate (Child-Pugh B): Reduce starting dose by 75%

  • Severe (Child-Pugh C): Contraindicated

Ethnic Considerations:

  • East Asian patients: Start at 50% reduced dose

  • Consider genetic testing for UGT1A1 polymorphisms

Pediatric Use:

  • Safety established down to 1 year old

  • Use oral suspension for children <25 kg

6. Adverse Effects

Common (≥10%):

  • Headache (22%)

  • Nausea (13%)

  • Fatigue (12%)

  • Upper respiratory infection (11%)

  • ALT elevation (10%)

Serious (Require Monitoring):

  • Hepatotoxicity (2.5%)

  • Thromboembolism (3%)

  • Bone marrow fibrosis (long-term use)

  • Cataract formation

7. Drug Interactions

Interacting Drug Effect Management
Polyvalent cations (Ca, Mg, Al, Fe) ↓ Absorption Separate by 4+ hours
CYP1A2 inhibitors (fluvoxamine) ↑ Eltrombopag levels Monitor for toxicity
CYP2C8 inducers (rifampin) ↓ Efficacy Consider dose increase
Statins ↑ Myopathy risk Monitor CK levels

8. Monitoring Requirements

Baseline:

  • CBC with platelet count

  • Liver function tests

  • Renal function

  • Ophthalmologic exam

  • Bone marrow biopsy (if long-term use anticipated)

Ongoing:

  • Weekly platelet counts until stable

  • LFTs every 2 weeks ×2 months, then monthly

  • Regular blood pressure monitoring

  • Annual:

    • Eye exams

    • Bone marrow evaluation (if chronic use)

9. Storage & Handling

  • Store at 20-25°C (68-77°F)

  • Keep in original packaging (moisture sensitive)

  • Protect from light

  • Shelf life: 24 months unopened

10. Cost & Availability

  • Brand Name Cost: ~$4,500/month

  • Generic Availability: Limited (check local formularies)

  • Patient Assistance Programs: Available through manufacturer

11. Clinical Pearls

  1. Dose Adjustment Triggers:

    • Platelets >150,000/μL: Reduce dose

    • Platelets >400,000/μL: Hold dose

    • No response after 4 weeks: Discontinue

  2. Transitioning Between Formulations:

    • 25 mg tablet ≈ 24 mg oral suspension

    • Monitor platelets closely when switching

  3. Overdose Management:

    • Symptomatic treatment

    • Monitor for thrombocytosis

    • Consider plateletpheresis if platelets >1,000,000/μL

  4. Discontinuation Protocol:

    • Taper gradually to avoid thrombocytopenia rebound

    • Monitor platelets for ≥4 weeks post-discontinuation

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. Definition & Pharmacological Class

  • Generic Name: Eltrombopag olamine

  • Therapeutic Category: Thrombopoietin receptor agonist (TPO-RA)

  • Mechanism of Action:

    • Binds to transmembrane domain of TPO receptor

    • Stimulates JAK2/STAT5 pathway → megakaryocyte proliferation

    • Increases platelet production in bone marrow

2. Approved Indications

✅ FDA/EMA Approved Uses:

  1. Chronic Immune Thrombocytopenia (ITP)

    • Adults and children ≥1 year

    • Second-line after corticosteroids/IVIG failure

  2. Severe Aplastic Anemia (SAA)

    • In combination with immunosuppressants

  3. Hepatitis C-Associated Thrombocytopenia

    • Enables interferon-based antiviral therapy

🚫 Important Limitations:

  • Not for first-line ITP treatment

  • Contraindicated in myelodysplastic syndromes

  • Not approved for chemotherapy-induced thrombocytopenia

3. Pharmacokinetics

Parameter Value Clinical Significance
Bioavailability 52% Reduced with food
Tmax 2-6 hours Take on empty stomach
Half-life 26-35 hours Once daily dosing
Protein binding >99% Caution in hepatic impairment
Metabolism Hepatic (CYP1A2/CYP2C8) Drug interaction potential
Excretion Fecal (59%), renal (31%) Dose adjustment not needed for renal impairment

4. Dosage & Administration

Standard Dosing Guidelines:

Indication Starting Dose Titration Maximum Dose
Adult ITP 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (6-17 yrs) 25 mg once daily ↑ by 25 mg every 2 weeks 75 mg/day
Pediatric ITP (1-5 yrs) 12.5 mg once daily ↑ by 12.5 mg every 2 weeks 75 mg/day
SAA 50 mg once daily* Adjust based on response 150 mg/day
HCV Thrombocytopenia 25 mg once daily ↑ weekly as needed 100 mg/day

Administration Instructions:

  • Take 1 hour before or 2 hours after meals

  • Avoid concomitant:

    • Dairy products (separate by ≥4 hours)

    • Polyvalent cation-containing medications (antacids, iron supplements)

  • Swallow tablet whole with water

5. Special Populations

Hepatic Impairment:

  • Mild (Child-Pugh A): Reduce starting dose by 50%

  • Moderate (Child-Pugh B): Reduce starting dose by 75%

  • Severe (Child-Pugh C): Contraindicated

Ethnic Considerations:

  • East Asian patients: Start at 50% reduced dose

  • Consider genetic testing for UGT1A1 polymorphisms

Pediatric Use:

  • Safety established down to 1 year old

  • Use oral suspension for children <25 kg

6. Adverse Effects

Common (≥10%):

  • Headache (22%)

  • Nausea (13%)

  • Fatigue (12%)

  • Upper respiratory infection (11%)

  • ALT elevation (10%)

Serious (Require Monitoring):

  • Hepatotoxicity (2.5%)

  • Thromboembolism (3%)

  • Bone marrow fibrosis (long-term use)

  • Cataract formation

7. Drug Interactions

Interacting Drug Effect Management
Polyvalent cations (Ca, Mg, Al, Fe) ↓ Absorption Separate by 4+ hours
CYP1A2 inhibitors (fluvoxamine) ↑ Eltrombopag levels Monitor for toxicity
CYP2C8 inducers (rifampin) ↓ Efficacy Consider dose increase
Statins ↑ Myopathy risk Monitor CK levels

8. Monitoring Requirements

Baseline:

  • CBC with platelet count

  • Liver function tests

  • Renal function

  • Ophthalmologic exam

  • Bone marrow biopsy (if long-term use anticipated)

Ongoing:

  • Weekly platelet counts until stable

  • LFTs every 2 weeks ×2 months, then monthly

  • Regular blood pressure monitoring

  • Annual:

    • Eye exams

    • Bone marrow evaluation (if chronic use)

9. Storage & Handling

  • Store at 20-25°C (68-77°F)

  • Keep in original packaging (moisture sensitive)

  • Protect from light

  • Shelf life: 24 months unopened

10. Cost & Availability

  • Brand Name Cost: ~$4,500/month

  • Generic Availability: Limited (check local formularies)

  • Patient Assistance Programs: Available through manufacturer

11. Clinical Pearls

  1. Dose Adjustment Triggers:

    • Platelets >150,000/μL: Reduce dose

    • Platelets >400,000/μL: Hold dose

    • No response after 4 weeks: Discontinue

  2. Transitioning Between Formulations:

    • 25 mg tablet ≈ 24 mg oral suspension

    • Monitor platelets closely when switching

  3. Overdose Management:

    • Symptomatic treatment

    • Monitor for thrombocytosis

    • Consider plateletpheresis if platelets >1,000,000/μL

  4. Discontinuation Protocol:

    • Taper gradually to avoid thrombocytopenia rebound

    • Monitor platelets for ≥4 weeks post-discontinuation

Reviews

There are no reviews yet.

Be the first to review “REBOPAG 25”

Your email address will not be published. Required fields are marked *

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